Abstract
The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597), a renin inhibitor with a suitable profile for development is described.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Angiotensinogen / genetics
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Animals
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Animals, Genetically Modified
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme Inhibitors
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Indicators and Reagents
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Models, Molecular
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology*
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Rats
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Renin / antagonists & inhibitors*
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Renin / genetics
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cytochrome P-450 Enzyme Inhibitors
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Enzyme Inhibitors
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Indicators and Reagents
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Piperidines
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Angiotensinogen
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Cyp3a2 protein, rat
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Cytochrome P-450 CYP3A
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Renin